Receptor antagonist
    4.
    发明申请
    Receptor antagonist 审中-公开
    受体拮抗剂

    公开(公告)号:US20070117840A1

    公开(公告)日:2007-05-24

    申请号:US10549889

    申请日:2004-03-16

    IPC分类号: A61K31/4704

    CPC分类号: A61K31/4704

    摘要: A compound represented by the formula (I): wherein ring A represents an aromatic ring; X represents a bond, oxygen, NR4 (R4 represents hydrogen, a hydrocarbon group, or a heterocyclic group), or alkylene; R1 represents a hydrocarbon group, or a heterocyclic group; R2 represents —COYR5 (Y represents a bond, alkylene, oxygen, sulfur, or NR6 (R6 represents hydrogen, a hydrocarbon group, or a heterocyclic group), and R5 represents a hydrocarbon group, or a heterocyclic group), a hydrocarbon group, or a heterocyclic group; and R3 represents a hydrocarbon group, a heterocyclic group, optionally substituted hydroxy, optionally substituted amino, or —S(O)nR7 (R7 represents a hydrocarbon group, or a heterocyclic group, and n is 0 to 2), a salt of the compound, or a prodrug or either is useful as an agent for modulating the function of an RFRP receptor.

    摘要翻译: 由式(I)表示的化合物:其中环A表示芳环; X表示键,氧,NR 4(R 4表示氢,烃基或杂环基)或亚烷基; R 1表示烃基或杂环基; R 2表示-COYR 5(Y表示键,亚烷基,氧,硫或NR 6(R 6) SUP>表示氢,烃基或杂环基),R 5表示烃基或杂环基),烃基或杂环基; 和R 3表示烃基,杂环基,任选取代的羟基,任选取代的氨基或-S(O)n R 7 (R 7表示烃基或杂环基,n为0〜2),化合物或前药的盐或其可用作调节其功能的试剂 RFRP受体。

    Use of peptide
    6.
    发明授权
    Use of peptide 失效
    使用肽

    公开(公告)号:US07045497B1

    公开(公告)日:2006-05-16

    申请号:US09868885

    申请日:1999-12-22

    CPC分类号: A61K38/2257

    摘要: The present invention relates to use of peptide to which G-protein coupled receptor protein recognizes as a ligand. Since the ligand polypeptide of the present invention has a stimulating action on oxytocin secretion, it is useful as a drug for ameliorating, preserving or treating various diseases related to oxytocin secretion such as uterine inertia, atonic hemorrhage, placental expulsion, subinvolution and the like.

    摘要翻译: 本发明涉及G蛋白偶联受体蛋白识别为配体的肽的用途。 由于本发明的配体多肽对催产素分泌具有刺激作用,因此可用作改善,保存或治疗与催产素分泌相关的各种疾病如子宫惯性,失声性出血,胎盘排出,亚溶解等的药物。

    Polypeptides their production and use
    8.
    发明授权
    Polypeptides their production and use 失效
    多肽的生产和使用

    公开(公告)号:US06228984B1

    公开(公告)日:2001-05-08

    申请号:US08776971

    申请日:1997-02-07

    IPC分类号: C07K1447

    摘要: The present invention relates to the ligand polypeptide for the human pituitary- and mouse pancreas-derived G protein-coupled receptor proteins. The ligand polypeptide or the DNA which codes for the ligand polypeptide can be used for (1) development of medicines such as pituitary function modulators, central nervous system function modulators, and pancreatic function modulators, and (2) development of recombinant receptor proteins and screening of pharmaceutical candidate compounds. In particular, by the receptor binding assay systems utilizing the expression of recombinant G protein-coupled receptor proteins in accordance with the invention, agonists and antagonists of G protein-coupled receptors which are specific to human and other warm-blooded animals can be screened and the agonists or antagonists obtained can be used as therapeutic and prophylactic agents for various diseases.

    摘要翻译: 本发明涉及用于人垂体和小鼠胰腺衍生的G蛋白偶联受体蛋白质的配体多肽。 编码配体多肽的配体多肽或DNA可用于(1)开发药物如垂体功能调节剂,中枢神经系统功能调节剂和胰腺功能调节剂,以及(2)重组受体蛋白的发育和筛选 的药物候选化合物。 特别地,通过利用根据本发明的重组G蛋白偶联受体蛋白表达的受体结合测定系统,可以筛选对人类和其他温血动物特异性的G蛋白偶联受体的激动剂和拮抗剂, 获得的激动剂或拮抗剂可用作各种疾病的治疗和预防剂。

    Fused proteins comprising glycoprotein gD of HSV-1 and LTB
    9.
    发明授权
    Fused proteins comprising glycoprotein gD of HSV-1 and LTB 失效
    包含HSV-1和LTB的糖蛋白gD的融合蛋白

    公开(公告)号:US5241053A

    公开(公告)日:1993-08-31

    申请号:US577915

    申请日:1990-09-05

    摘要: Disclosed are (1) a fused protein comprising heat-labile enterotoxin B subunit and a protein heterologous to heat-labile enterotoxin, (2) a recombinant DNA containing a nucleotide sequence coding for the above fused protein, (3) a transformant harboring the above recombinant DNA, (4) a method for producing the fused protein which comprises cultivating the above transformant, producing and accumulating the above fused protein in a culture, and collecting the fused protein, and (5) a method for purifying a fused protein comprising a herpes simplex virus surface antigen and heat-labile enterotoxin B subunit, which comprises cultivating a transformant harboring a recombinant DNA containing a nucleotide sequence coding for the fused protein, producing an accumulating the fused protein in a culture, collecting the fused protein and subjecting the collected fused protein to purification processes comprising cationic exchange chromatography and gel permeation chromatography.

    摘要翻译: 公开了(1)包含热不稳定肠毒素B亚基和与热不稳定肠毒素异源的蛋白质的融合蛋白,(2)含有编码上述融合蛋白的核苷酸序列的重组DNA,(3)含有上述 重组DNA,(4)生产融合蛋白的方法,包括培养上述转化体,在培养物中产生和积累上述融合蛋白,并收集融合蛋白,和(5)纯化融合蛋白的方法, 单纯疱疹病毒表面抗原和热不稳定肠毒素B亚基,其包括培养含有编码融合蛋白的核苷酸序列的重组DNA的转化体,产生在培养物中积聚融合蛋白,收集融合蛋白并使收集的 融合蛋白与包含阳离子交换层析和凝胶渗透色谱的纯化方法。

    Methods of screening for compounds which bind G protein-coupled receptors
    10.
    发明授权
    Methods of screening for compounds which bind G protein-coupled receptors 失效
    筛选结合G蛋白偶联受体的化合物的方法

    公开(公告)号:US07927821B2

    公开(公告)日:2011-04-19

    申请号:US11578325

    申请日:2005-04-11

    摘要: The present invention provides a method of screening an agonist or antagonist to a G protein-coupled receptor protein comprising the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1, or a salt thereof, which comprises using the receptor protein or a salt thereof and the ligand or a salt thereof; etc. The present invention is useful for screening agents for the prevention/treatment of, e.g., leukopenia, leukemia, lymphoma, malignant tumor, ulcerative colitis, rheumatoid arthritis, inflammatory bowel disorders, tonsil disorders, collagen disease, inflammatory disease, leukocytosis, heart failure, inherited muscle disorders, muscular dystrophy, neuromuscular degenerative disease, myocardial infarction, obesity, mellitus diabetes, hyperlipemia, arteriosclerosis, metabolic syndrome, thrombocytopenia, thrombocytosis, cancer, pulmonary edema, multiple organ failure, etc.

    摘要翻译: 本发明提供筛选G蛋白偶联受体蛋白的激动剂或拮抗剂的方法,其包含与SEQ ID NO:1所示的氨基酸序列相同或基本上相同的氨基酸序列,或其盐,其包含 使用受体蛋白或其盐和配体或其盐; 本发明可用于预防/治疗例如白细胞减少症,白血病,淋巴瘤,恶性肿瘤,溃疡性结肠炎,类风湿性关节炎,炎性肠病,扁桃体病,胶原病,炎性疾病,白细胞增多症,心脏病 失败,遗传性肌肉疾病,肌营养不良症,神经肌肉退行性疾病,心肌梗死,肥胖症,糖尿病,高脂血症,动脉硬化,代谢综合征,血小板减少症,血小板增多症,癌症,肺水肿,多器官衰竭等。